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Injectable long-acting analgesic composition comprising an ester derivative of ketorolac

an analgesic composition and ester derivative technology, applied in the direction of drug compositions, heterocyclic compound active ingredients, biocide, etc., can solve the problems of severe acute pain, no known ketorolac esters applied, and the short-term management of severe pain and acute pain of ketorolac tromethamine, etc., to achieve the effect of prolonging the anti-inflammatory

Inactive Publication Date: 2006-08-17
CHI MEI MEDICAL CENT
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0022] As compared to ketorolac or ketorolac tromethamine, the composition according to this invention can provide a longer duration of action and, therefore, is suitable for use in the treatment of long-lasting pains and inflammations.

Problems solved by technology

However, in other cancer patients, morphine was more effective than ketorolac but less well tolerated (M. M. T. Buckley et al.
However, to the applicant's knowledge, none of the known ketorolac esters was applied for a purpose of long-acting effect.
However, like ketorolac, ketorolac tromethamine can only provide short-term (up to 5 days) management of severe, acute pains that require analgesia at the opiate level.
It may cause severe side effects if taken for a longer time.

Method used

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  • Injectable long-acting analgesic composition comprising an ester derivative of ketorolac
  • Injectable long-acting analgesic composition comprising an ester derivative of ketorolac
  • Injectable long-acting analgesic composition comprising an ester derivative of ketorolac

Examples

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examples

[0074] Table 1 shows the chemical structures of the preferred ketorolac ester derivatives obtained in the following Synthesis Examples.

TABLE 1The chemical structures of ketorolac, ketorolac tromethamine, andketorolac ester derivatives obtained in the Synthesis Examples.Compound nameChemical structureKetorolacKeto—HKetorolacKeto.TromethaminetromethamineKetorolac propyl esterKetorolac pentyl esterKetorolac tert-butyl esterKetorolac hexyl esterKetorolac heptyl esterKetorolac decyl esterKetorolac cetyl esterKetorolac benzyl ester

[0075] The ketorolac ester derivatives listed in Table 1 can be synthesized by suitable known methods other than those described below.

Synthesis Ex. 1

Preparation of Ketorolac Propyl Ester

[0076] Ketorolac tromethamine was purchased from Sigma (Saint Louis, Mo., USA). Ketorolac was obtained from its tromethamine salt using a precipitation method. Following adding 1 N HCl drop by drop into a ketorolac tromethamine solution, ketorolac was precipitated. The coll...

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Abstract

Disclosed herein is an injectable long-acting analgesic composition comprising: (a) a ketorolac ester derivative of formula (I),  wherein  R is a straight-chain or branched saturated or unsaturated C1-C20 aliphatic group optionally substituted with a C6-C10 aryl group; and (b) a pharmaceutically acceptable oil vehicle. The composition can provide a longer duration of action and, therefore, is suitable for use in the treatment of long-lasting pains and inflammations.

Description

BACKGROUND OF THE INVENTION [0001] 1. Field of the Invention [0002] This invention relates to an injectable long-acting analgesic composition comprising an ester derivative of ketorolac and a pharmaceutically acceptable oil vehicle. [0003] 2. Description of the Related Art [0004] Most patients who experience moderate to severe pain, such as post-operative pain, post-traumatic pain and burn pain, often require pain control in the first 3 days after injury. An analgesic with a long-acting effect of around 3 days may be particularly valuable for this purpose (K.-S. Chu, et al. (2003), Anesthesia Analgesia, Vol. 97, 806-809). Currently, nonsteroidal anti-inflammatory drugs (NSAIDs) are often used in this field (J. C. Grillis et al. (1997), ADIS Drug Evaluation, Vol. 53, 139-188), but all of them are short-acting drugs. Prolonging the duration of action would make NSAIDs, e.g., a potent NSAID, more valuable in treating long-lasting pains clinically. [0005] Amongst NSAIDs, ketorolac is th...

Claims

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Application Information

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IPC IPC(8): A61K31/407
CPCA61K31/407A61P29/00
Inventor WANG, JHI-JOUNG
Owner CHI MEI MEDICAL CENT
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